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Describe the 4 major eicosanoid receptors and their signaling pathways:
- Relaxant: Gs - IP, EP2, EP4, DP1
- Contractile: Gq, G12/13 (rho) and G16 - TP, FP, EP
- Inhibitory: Gi - EP3
- fMLP Receptor Family: Gi - DP2/CRH2
What are the 3 major inflammatory functions of prostaglandins:
- Pain: Hypealgesia by sensitizing neurons to bradykinin, histamine, 5-HT and substance P
- Heat/Redness Production: PGE2 and PGI2
- Swelling: Extravasation of fluid by other mediators
Describe the effect of Prostacyclin (PGI2) on platelets? Where is it produced?
- Produced by: Endothelium
- Function: Inhibit aggregation, contribute to antithrombotic properties of endothelium and produce vasodilation
What is the effect of Thromboxane (TXA2) on platelets? Where is it produced?
- Prodyced by: Platelets
- Function: Promote aggregation of platelets and produce vasoconstriction
Describe the function of prostaglandins in the female reproductive system?
- Non-Pregnant: PGF2 contracts uterus and causes CL regression, while PGE2 relaxes uterus
- Pregnant: BOTH PGE2 and PGF2 contract uterus and PGF2 is important in parturition
- In pregnancy, both levels continue to increase in amniotic fluid and blood
Describe the functionof prostaglandins in the male reproductive tract? Where is it produced?
- Produced in: Seminal vesicle, high amt found in semen
- May help contraception by acting on cervix, uterine body, fallopian tubes
- Low levels may correlate with infertility
Describe the function of prostaglandins in the kidney?
Function: Modulate blood flow, regulate urine and renin secretion
Describe the SPECIAL function of PGE2 in the kidney
- Vasodilate afferent arterioles
- Lower sodium reabsorption
- Increase renin scretion
Describe the PG function in GI system? Which PG are especially important?
- Function: Increase mucus secretion and water movement into lumen
- PGE2 and PGI2: Inhibit vgastric acid secretion and produce vasodilation of gastric mucosa
What PG are especially important in the pulmonary system? What is their function?
- PGF2, PGD2 and TXA2: Contract bronchial smooth muscle
- PGE1, PGE2, PGI2: Relax bronchial smooth muscle
Describe function of PGE2 in CNS?
- Increased in anterior HT by pyogens
- Vasodilation in cerebral blood vessels (headache?)
What prostaglandins are used in treatment of glaucoma?
What drugs are used in gastric/duodenal ulcer treatment?
- Misoprost/Diclocfenac - with high NSAID use
What drugs are used for early abortion induction?
What drugs are used for postpartum hemorrhage?
What drugs are used for labor induction?
What drugs are used to maintain the patency of DA?
What drugs are used for ED?
What drugs are used to treat pulmonary hypertension?
What conditions are treated using prostaglandins?
- Gastric/Duodenal Ulcers
- Abortions (week 13-20)
- Postpartum hemorrhage
- Labor induction
- Patency of ductus arteriosis
- Erectile Dysfunction
- Pulmonary hypertension
Describe the effect of leukotrienes in the CV system - coronary and pulmonary arteries, endothelium permeability?
- Coronary Artery: Constriction - may be responsible for coronary artery vasospasms, cardiac anaphylaxis
- Pulmonary Artery: Constriction
- Endothelium: Increased permeability, exudation into tissue
- Mediator of endotoxic shock
What is a major function of LTB4 as pertaining to neutrophils, eosinophils and monocytes?
- Promote PMN aggregation
- Degranulation at higher concentrations
What is the major funciton of LT in pulmonary system? Which one are important?
- LTC4 and LTD4: Important in asthma and hypersensitivity
- Made by mast cells
- Vasoconstriction, mucus secretion, edema
What is the major function of LT in renal system?
- Reduced GFR
- May produce acute glomerular nephritis
Describe mechanism, uses, S/E and special condsideration of Zafirlukast (Accolate)
- Mechanism: LTD4 and LTE4 antagonist, inhibit bronchoconstriction
- Use: Maintenance therapy for chronic asthma
- S/E: Heaache, GI distrubance, pharyngitis, cough, rhinitis
- Special: Metabolized by CYP2C9, weakly inhibits CYP3A4 and CYP2C9
- Slow onset of action - caution in patients with liver disease
Describe mechanism, uses, S/E and special condsideration of Montelukast (Singulair)
- Mechanism: LTD4 receptor antagonist, inhibit bronchoconstriction
- Use: Maintenace therapy for chronic asthma, exercise-induced asthma
- S/E: Headache, cough, suicide, mood changes
- Special: Metabolized by CYP3A4 and CYP2C9 but DOES NOT inhibit P450
- Be careful of patients with aspirin-sensitive asthma
Describe mechanism, uses, S/E and special condsideration of Zileuton (Zyflo)
- Mechanism: 5-Lipoxygenase inhibitor, block ALL LT synthesis
- Use: Maintenance therapy for chronic asthma
- S/E: Dyspnea, flu-like symptoms, rare hepatitis
- Special: Inhibits P450 system, monitor liver function
What is the function of platelet activating factor in the pulmonary system?
Longterm bronchoconstriction - may last 4 weeks
What is the funciton of PAF in CV system?
Hypotension independent of sympathetic tone
What are some other functions of PAF?
- Platelet aggregation
- Leukocyte chemotaxis
- IV-PAF resembles anaphylaxis
- PAF generation = successful implantation and pregnancy
What are potential pathophysiological functions of PAF?
- Shock (hypotension)
- Asthma (bronchoconstriction)
- Inflammation - chemotaxis, degranulation, vasodilation
- Graph rejection